Ceftriaxone sodium

Ceftriaxone sodium

Class:Antibiotic,cephalosporin (third generation)

Mechanism of action

Inhibit bacterial cell wall synthesis by binding to one or more of the penicillin binding proteins(PBPs) which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell wall,.Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes(autolysins and murein hydrolases) while cell wall assembly is arrested.

Pharmacokinetics

Absorption:IM:well absorbed.Distribution:widely distributed throughout the body including gallbladder,lungs,bone,bile,CSF,crosses placenta,reaches amniotic fluid and milk.Protein binding 85 to 95 percent.Half life 5-9 hours.Peak serum concentration:IM;within 1-2 hours.Elimination:excreted unchanged in urine by glomerular filtration and in feces.

Indications

Severe respiratory and genito UTIs,bone and joint infections,abdominal infections,sepsis and meningitis.

Contraindications

Hypersensitivity to any component,or cephalosporins;donot use in hyperbillirubinemic neonates,particularly those who are premature since ceftriaxone is reported to displace bilirubin from albumin binding sites.

Precautions

Prolong use may result in superinfection,use with caution,a history of penicillin allergy,especially IgE-mediated reactions(e.g anaphylaxis,urticaria);may cause antibiotic associated colitis or colitis secondary to C.difficile.

Side effects

Pain at injection site,hypersensitivity reaction,GI disturbances,candidiasis,thrombocytopenia,rise in liver enzymes and blood urea.positive comb’s test.

Pregnancy

Pregnancy risk factor B

Drug interactions

Increased effect:aminoglycoside may result in synergistic antibacterial activity.High dose probenecid decreases clearance.Increased toxicity:aminoglycoside increase nephrotoxic potential.

Dosage

Adults:usually 1 gm daily by deep IM,slow IV inj.over atleast 2-4 minutes.,or IV inf.Severe infection:2-4 gm as a single dose every 24 hrs.Gonorrhea,single dose of 250 mg by IM inj.Children usually 20-50 mg/kg once daily by IM inj.,slow IV inj.over atleast 2-4 minutes.,or IV infusion,upto max. 80mg/kg daily.doses over 50 mg/kg to be given by slow IV inf.over atleast 30 minutes.

Brands

Inj.Oxidil 250,500 mg,inj.Rocephen 250,500 mg.